Supportive measures and symptomatic treatment, with gastric lavage if necessary, may be adequate.
Fluconazole is largely excreted in the urine and therefore, forced volume diuresis would probably increase the elimination rate. Plasma levels are decreased by approximately 50% during a 3-hour haemodialysis session.
3 years
Known hypersensitivity to fluconazole, related azole compounds or any of the excipients in this product.
Fluconazole should not be administered concomitantly with terfenadine, cisapride or ergot-derivatives (see 4.5).
Not applicable
Lactose monohydrate
Maize starch
Colloidal silicon dioxide
Magnesium stearate
Sodium lauryl sulphate
Capsule shells contain:
Brilliant blue FCF (E133)
Titanium dioxide (E171)
Gelatin
Printing ink contains:
Shellac
Black iron oxide (E172)
Propylene glycol
Hard capsule
Opaque light blue capsule (size 1) with "Canesten®" printed in black between two black lines.
The listed undesirable effects are based on spontaneous reports, thus an organisation according to CIOMS III categories of frequency is not possible.
Blood and lymphatic system disorders
Leukopenia, neutropenia, agranulocytosis, thrombocytopenia.
Cardiac disorders
Torsades de pointes/QT prolongation.
Gastrointestinal disorders
Nausea, diarrhea, vomiting, gastrointestinal and abdominal pains, abdominal distension, flatulence.
Hepatobiliary disorders
Most events were observed when a multiple treatment was used: mild transient elevations in transaminases, hepatitis (non infective), jaundice, cholestasis and acute hepatic failure, including fatalities.
Immune System Disorders
Allergic reaction, anaphylactic reaction, anaphylactic shock.
Hypersensitivity reactions including symptoms such as rash, urticaria, oedema, pruritus, cardio-respiratory distress.
Investigations
Electrocardiogram QT prolonged, electrocardiogram QT corrected interval prolonged, hypercholesterolemia, hypertriglyceridemia, hypokalemia.
Nervous system disorders
Seizures, dizziness, headache, dysgeusia.
Skin and subcutaneous tissue disorders
Rash, pruritus, alopecia, exfoliative skin reactions including Stevens-Johnson syndrome, toxic epidermal necrolysis.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.
Reproductive Toxicity:
At 25 and 50mg/kg and higher doses, increases in foetal anatomical variants (supernumerary ribs, renal pelvis dilation) and delays in ossification were observed. At doses ranging from 80mg/kg to 320mg/kg embryolethality in rats was increased and foetal abnormalities included wavy ribs, cleft palate and abnormal cranio-facial ossification. This may be a result of known effects of lowered oestrogen on pregnancy, organogenesis and parturition as it is consistent with the inhibition of oestrogen synthesis in rats.
Carcinogenesis:
No evidence of carcinogenic potential was observed in mice and rats treated orally with fluconazole for 24 months at doses of 2.5, 5 or 10mg/kg/day. The incidence of hepatocellular adenomas was increased in male rats treated with 5 and 10mg/kg/day.
Mutagenesis:
Fluconazole, with or without metabolic activation, was negative in tests for mutagenicity in 4 strains of S. typhimurium and in the mouse lymphoma L5178Y system. No evidence of chromosomal mutations was observed in cytogenetic studies in vivo (murine bone marrow cells, following oral administration of fluconazole). Data derived from in vitro studies (human lymphocytes exposed to fluconazole) are not consistent.
Impairment of Fertility:
The fertility of male or female rats treated orally with daily doses of fluconazole at doses of 5, 10 or 20mg/kg or with parenteral doses of 5, 25 or 75mg/kg was not affected, although the onset of parturition was slightly delayed at 20mg/kg p.o. In an intravenous perinatal study in rats at 5, 20 and 40mg/kg, dystocia and prolongation of parturition were observed in a few dams at 20mg/kg and 40mg/kg, but not at 5mg/kg. The disturbances in parturition were reflected by a slight increase in the number of stillborn pups and decrease of neonatal survival at these dose levels. The effects on parturition in rats are consistent with the species specific oestrogen-lowering property produced by high doses of fluconazole. Such a hormone change has not been observed in women treated with fluconazole.
Canesten Thrush Oral Capsule is recommended for the treatment of candidal vaginitis, acute or recurrent. It should also be used for the treatment of partners with associated candidal balanitis.
Pharmacotherapeutic group: Fluconazole is a triazole antifungal, ATC-Code: J02AC01
Fluconazole is a triazole antifungal. It is a potent and selective inhibitor of fungal enzymes necessary for the synthesis of ergosterol.
Fluconazole shows little pharmacological activity in a wide range of animal studies. Some prolongation of pentabarbitone sleeping times in mice (p.o.), increased mean arterial and left ventricular blood pressure and increased heart rate in anaesthetised cats (i.v.) occurred. Inhibition of rat ovarian aromatase was observed at high concentrations.
Fluconazole was active in a variety of animal fungal infection models. Activity has been demonstrated against opportunistic mycoses, such as infections with Candida spp. including systemic candidiasis in immuno-compromised animals; with Cryptococcus neoformans, including intracranial infections; with Microsporum spp. and with Trichophyton spp. Fluconazole has also been shown to be active in animal models of endemic mycoses, including infections with Blastomyces dermatitides; with Coccidoides immitis, including intracranial infection and with Histoplasma capsulatum in normal and immuno-compromised animals.
There have been reports of cases of superinfection with Candida species other than C. albicans, which are often inherently not susceptible to fluconazole (e.g. Candida krusei). Such cases may require alternative antifungal therapy.
Fluconazole is highly specific for fungal cytochrome P-450 dependent enzymes. Fluconazole has been shown not to affect testosterone plasma concentrations in males or steroid concentrations in females of childbearing age when given 50mg daily for up to 28 days. No clinically significant effect has been seen on endogenous steroid levels or on ACTH stimulated response in healthy male volunteers taking fluconazole 200 - 400mg daily. Interaction studies with antipyrine indicate that single or multiple doses of fluconazole 50mg do not affect its metabolism.
The pharmacokinetic properties of fluconazole are similar whether administered orally or by the intravenous route. After oral administration, fluconazole is well absorbed and plasma levels (and systemic bioavailability) are over 90% of the levels achieved after intravenous administration. Concomitant food intake does not affect oral absorption. In the fasting state peak plasma concentrations occur between 0.5 and 1.5 hours post-dose with a plasma elimination half-life of approximately 30 hours. Plasma concentrations are proportional to dose. Ninety- percent steady state levels are reached by day 4 to 5 with multiple once daily dosing.
Administration of a loading dose (on day 1) of twice the usual daily dose enables plasma levels to approximate to 90% steady state levels by day 2. The apparent volume of distribution approximates to total body water. Plasma protein binding is low (11-12%).
Fluconazole achieves good penetration in all body fluids studied. The levels of fluconazole in saliva and sputum are similar to plasma levels. In patients with fungal meningitis, fluconazole levels in the CSF are approximately 80% of the corresponding plasma levels.
High skin concentrations of fluconazole, above serum concentrations, are achieved in the stratum corneum, epidermis-dermis and eccrine sweat. Fluconazole accumulates in the stratum corneum. At a dose of 50mg once daily, the concentration of fluconazole after 12 days was 73 mg/g and 7 days after cessation of treatment the concentration was still 5.8 mg/g.
Excretion is mainly renal, with approximately 80% of the administered dose appearing in the urine as unchanged drug. Fluconazole clearance is proportional to creatinine clearance. There is no evidence of circulating metabolites.
The long plasma elimination half-life provides the basis for single dose therapy for genital candidiasis.
A study compared the saliva and plasma concentrations of a single fluconazole 100mg dose administration in a capsule or in an oral suspension by rinsing and retaining in the mouth for 2 minutes and swallowing. The maximum concentration of fluconazole in saliva after the suspension was observed five minutes after ingestion and was 182 times higher than maximum saliva concentration after the capsule which occurred four hours after ingestion. After about four hours, the saliva concentrations of fluconazole were similar. The mean AUC (0-96) in saliva was significantly greater after the suspension compared to the capsule. There was no significant difference in the elimination rate from the saliva or the plasma pharmacokinetic parameters for the two formulations.
09 August 2017
Canesten Thrush Oral Capsule 150mg capsule
Bayer plc
Bayer House
Strawberry Hill
Newbury
Berkshire
RG14 1JA
U.K.
Trading as Bayer plc, Consumer Care Division
No special precautions for storage
Opaque, white PVC/PVdC (60g/m2) blister with 20µm aluminium foil backing containing one capsule.
PL 00010/0282
Fluconazole 150mg
For excipients, see 6.1
The product available from pharmacies without prescription will include a leaflet that advises the patient - Do not use Canesten Thrush Oral Capsule without first consulting your doctor:
If you are under 16 or over 60 years of age
If you are allergic to any of the ingredients in Canesten Thrush Oral Capsule or other antifungals and other thrush treatments (see section “After Taking Canesten Thrush Oral Capsuleâ€).
If you are taking any other medicine other than the Pill.
If you are taking the antihistamine terfenadine or the prescription medicine cisapride
If you have had thrush more than twice in the last six months
If you have any disease or illness affecting your liver or kidneys or have had unexplained jaundice.
If you suffer from any other chronic disease or illness.
If you or your partner have had exposure to a sexually transmitted disease.
If you are unsure of the cause of your symptoms.
Women only:
If you are pregnant, suspect you might be pregnant or are breast-feeding.
If you have any abnormal or irregular vaginal bleeding or a blood stained discharge
If you have vulval or vaginal sores, ulcers or blisters.
If you are experiencing lower abdominal pain or burning sensation on passing water.
Men only:
If your sexual partner does not have thrush.
If you have penile sores, ulcers or blisters.
If you have an abnormal penile discharge (leakage).
If your penis has started to smell.
If you have pain on passing urine.
The product should never be used again if the patient experiences a rash or anaphylaxis following the use of the drug.
Recurrent use (men and women): patients should be advised to consult their physician if the symptoms have not been relieved within one week of taking Canesten Thrush Oral Capsule. Canesten Thrush Oral Capsule can be used if the candidal infection returns after 7 days. However, if the candidal infection recurs more than twice within six months, patients should be advised to consult their physician.
Fluconazole has been associated with rare cases of serious hepatic toxicity, including fatalities primarily in patients with serious underlying medical conditions.
Fluconazole must be taken with particular care in patients with congenital or acquired QT prolongation and torsades de pointes or a history thereof, known cardiomyopathy, sinus bradycardia, cardiac arrhythmia, or are treated with a co-medication potentially leading to QT prolongation (see 4.5).
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
No studies on the effect on the ability to drive and use machines have been performed. However, undesirable effects such as dizziness have been observed. If dizziness occurs, patients should not drive or operate machines.
Adults (16 to 60):
One capsule should be swallowed whole.
Children (under 16):
Paediatric use is not recommended.
Elderly:
Not recommended in patients over 60.
Renal Impairment:
There is no separate dosage schedule in patients with renal impairment for single dose therapy.
Not applicable.
25 September 2002
